| Identification | Back Directory | [Name]
[3,3'-Bipyridine]-5-carboxamide, 6'-chloro-N-methyl-5'-[(phenylsulfonyl)amino]- | [CAS]
2377604-81-2 | [Synonyms]
CHMFL-PI4K-127
[3,3'-Bipyridine]-5-carboxamide, 6'-chloro-N-methyl-5'-[(phenylsulfonyl)amino]- | [Molecular Formula]
C18H15ClN4O3S | [MOL File]
2377604-81-2.mol | [Molecular Weight]
402.85 |
| Hazard Information | Back Directory | [Uses]
CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy[1]. | [in vivo]
CHMFL-PI4K-127 (compound 15g) (Orally; 0-80 mg/kg/day for 7 days; 0-15 mg/kg, once) exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model[1]. | Animal Model: | Balb/c mice were infected by P. yoelii[1]. | | Dosage: | 0, 60, 80 mg/kg | | Administration: | Orally, daily for 7 days | | Result: | Displayed significant in vivo antimalarial activities in a dose-dependent manner and 80 mg/kg × 7 days treatment generated curative effects. The 60 mg/kg dosage resulted in suppressive effects during the drug treatment but relapsed after stopping treatment. |
| Animal Model: | Balb/c mice were infected by P. yoelii[1]. | | Dosage: | 0, 1, 5, 15 mg/kg | | Administration: | Orally, once | | Result: | Provided the full protection and cure at 1 mg/kg with no negligible parasite visible in the liver of all tested mice at 24, 48, 72, 96, 144 and 196 h, indicating true causal prophylactic efficacy. |
| [IC 50]
PI4K: 0.9 ± 0.1 nM (IC50); PI3Kδ: 104 ± 3 nM (IC50); PI3Kα: 191 ± 36 nM (IC50); PI3Kγ: 324 ± 19 nM (IC50); PI3Kβ: 392 ± 27 nM (IC50); Vps34: 681 ± 25 nM (IC50) | [References]
[1] 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium. Eur J Med Chem. 2020 Feb 15;1 DOI:10.1016/j.ejmech.2019.112012 |
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